The pyrrolo[2,3-d]pyrimidin-4-ones of the following formula 2, 3 and 4 ##STR1## 2, R is n-C.sub.3 H.sub.7 3, R is CH.sub.2 C.sub.6 H.sub.5
4, R is cyclopentyl
are known. R. K. Robins, et al, synthesized the compounds of formula 2 and 3 as reported in J. Het. Chem., 1964, 34, but gave no biological activity for either compound. M. Legraverend, et al, reported the synthesis of the compounds of formula 3 and 4 in Tetrahedron Letters, 1985, 2001, but again gave no biological activity for either compound.
Of lesser interest the following references provide a background in which a 7-(substituted phenyl)pyrrolo[2,3-d]pyrimidin-4-one having a methyl at each of the five (5) and six (6) positions for treating CNS illnesses or inflammations is disclosed generically in U.S. Pat. No. 4,229,453. Similarly, 4-mercapto-7-(phenyl substituted or unsubstituted)pyrrollo [2,3-d]pyrimidine derivatives requiring an alkyl or phenyl at the five (5) and six (6) positions are disclosed in German No. 3145287 (Derwent Abstract No. 49344 K/21). Other pyrrolo [2,3-d]pyrimidin-4-one or thione, distinguished by having various substituents at the five (5) position, are found in U.S. Pat. No. 4,435,570 and 4,140,851; European publications No. 160,910 (Derwent Abstract No. 85-284574/46); 89,055 (corresponding to U.S. Pat. No. 4,571,423); 119,591 (Derwent Abstract No. 84-238735/39); 79,447 (corresponding to U.S. Pat. No. 4,435,569); German No. 3,306-390 (Derwent Abstract No. 39438 E/20); German No. 3145287 (Derwent Abstract No. 49344 K/21); British Patent No. 981,458 (Derwent Abstract No. 15,454); Japanese No. J6 0204,788 (Derwent Abstract No. 85/298810/48); and Japanese No. J5 9036615 (Derwent Abstract No. 84-086061/84).
Finally, hydroxy and mercapto analogs of the antibiotic sparsomycin A are pyrrolo[2,3-d]pyrimidin-4-one or thione having a sugar moiety in the seven (7) position are disclosed by Upjohn in Netherlands No. 6,407,785 (Derwent Abstract No. 15,466) and similarly by Warner Lambert in European publication No. 57,548 (Derwent Abstract No. 68572 E/33).
Copending Applications Ser. No. 336,585, now U.S. Pat. No. 4,923,872, and Ser. No. 767,202 filed Aug. 22, 1985, now pending, which is a continuation-in-part of U.S. Ser. No. 660,152 filed Oct. 12, 1984, now abandoned, disclose similar activity as now found in the present invention for different ring systems.